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| Cas No.: | 130089-98-4 |
| Chemical Name: | 2-[(4-Acetylphenyl)amino]-3-chloro-1,4-naphthalenedione |
| Synonyms: | NQ 301, NQ-301 |
| SMILES: | CC(=O)C1=CC=C(C=C1)NC2=C(C(=O)C3=CC=CC=C3C2=O)Cl |
| Formula: | C18H12ClNO3 |
| M.Wt: | 325.75 |
| Purity: | >98% |
| Sotrage: | 4°C for 1 year, -20°C for more than 2 years |
| Description: | NQ301 is an antithrombotic agent; inhibits collagen-challenged rabbit platelet aggregation with an IC50 of 10 mg/mL. |
| Target: | IC50: 0.60±0.02 μM (collagen-challenged rabbit platelet aggregation), 0.58±0.04 μM (U46619-challenged rabbit platelet aggregation), 0.78±0.04 μM (arachidonic acid-challenged rabbit platelet aggregation)[1] |
| In Vitro: | NQ301 concentration-dependently inhibits collagen (10 mg/mL)-, U46619 (1 mg/mL)- and arachidonic acid (100 mg/mL)-challenged rabbit platelet aggregation, with IC50 values of 0.60±0.02, 0.58±0.04 and 0.78±0.04 μM, respectively. NQ301 potently suppresses thromboxane B2 formation by platelets that are exposed to arachidonic acid in a concentration-dependent manner, but had no effect on the production of prostaglandin D2, indicating an inhibitory effect on thromboxane A2 synthase. NQ301 has a potential to inhibit thromboxane A2 synthase activity with thromboxane A2/prostaglandin H2 receptor blockade, and modulate arachidonic acid liberation as well as 12-hydroxy-5,8,10,14-eicosatetraenoic acid formation in platelets[1]. NQ301 inhibits platelet aggregation by suppression of the intracellular pathway, rather than by direct inhibition of fibrinogen-GPIIb/IIIa complex binding. NQ301 significantly inhibits the increase of cytosolic Ca2+ concentration and ATP secretion, and also significantly increases platelet cAMP levels in the activated platelets. The antiplatelet activity of NQ301 may be mediated by inhibition of cytosolic Ca2+ mobilization, enhancement of cAMP production and inhibition of ATP secretion in activated platelets[2]. |
| Cell Assay: | ished rabbit platelet suspension is challenged by addition of collagen (10 mg/mL), arachidonic acid (100 μM) or U46619 (1 μM). Concentration- response relationship is determined in the absence or presence of a range of concentrations of NQ301 (0, 0.25, 0.5, 0.75, 1 μM); aspirin-treated platelets (50 μM for 5 min) are used to prevent any possible contribution of endogenous arachidonic acid metabolites to platelet aggregation. The resulting aggregation, measured as the change in light transmission, is recorded for 5 min. The extent of platelet aggregation is expressed as % of the control[1]. |
| References: | [1]. Jin YR, et al. An antithrombotic agent, NQ301, inhibits thromboxane A2 receptor and synthase activity in rabbit platelets. Basic Clin Pharmacol Toxicol. 2005 Sep;97(3):162-7. [2]. Zhang YH, et al. Antiplatelet effect of 2-chloro-3-(4-acetophenyl)-amino-1,4-naphthoquinone (NQ301): a possible mechanism through inhibition of intracellular Ca2+ mobilization. Biol Pharm Bull. 2001 Jun;24(6):618-22. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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